UNIT 1.3 Practical Aspects of Radioligand Binding

  1. Michael McKinney1,
  2. Rita Raddatz2

Published Online: 1 JUL 2006

DOI: 10.1002/0471141755.ph0103s33

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

McKinney, M. and Raddatz, R. 2006. Practical Aspects of Radioligand Binding. Current Protocols in Pharmacology. 33:1.3:1.3.1–1.3.42.

Author Information

  1. 1

    Mayo Clinic Jacksonville, Jacksonville, Florida

  2. 2

    Cephalon, Inc., West Chester, Pennsylvania

Publication History

  1. Published Online: 1 JUL 2006
  2. Published Print: JUN 2006


Radioligand binding has been used for many years to identify new binding sites, characterize receptors, and identify novel ligands. Although various techniques have been developed to improve the efficiency of preparing the biological source of the receptors and for detecting bound radioligand, the principles of the assays remain the same. This unit reviews theory and provides examples of the parameters that can be calculated from radioligand binding data to characterize ligand-receptor interactions. The important aspects of assay development and validation that allow meaningful interpretation are discussed. The selection of a radioligand, buffer and other assay components is critical to developing a useful binding assay. The nature of the binding interaction can also be probed by varying assay conditions.


  • radioligand binding;
  • filtration;
  • membrane preparation;
  • affinity;
  • saturation binding;
  • displacement